[HTML][HTML] The importance of cellular degradation kinetics for understanding mechanisms in targeted protein degradation

KM Riching, EA Caine, M Urh, DL Daniels - Chemical Society Reviews, 2022 - pubs.rsc.org
Targeted protein degradation has exploded over the past several years due to preclinical
and early clinical therapeutic success of numerous compounds, and the emergence of new …

Cellular resistance mechanisms to targeted protein degradation converge toward impairment of the engaged ubiquitin transfer pathway

P Ottis, C Palladino, P Thienger, A Britschgi… - ACS chemical …, 2019 - ACS Publications
Proteolysis targeting chimeras are bifunctional small molecules capable of recruiting a target
protein of interest to an E3 ubiquitin ligase that facilitates target ubiquitination followed by …

Structural basis for the selection of glycosylated substrates by SCFFbs1 ubiquitin ligase

T Mizushima, Y Yoshida… - Proceedings of the …, 2007 - National Acad Sciences
The ubiquitin ligase complex SCFFbs1, which contributes to the ubiquitination of
glycoproteins, is involved in the endoplasmic reticulum-associated degradation pathway. In …

The Prp19 U-box Crystal Structure Suggests a Common Dimeric Architecture for a Class of Oligomeric E3 Ubiquitin Ligases,

CW Vander Kooi, MD Ohi, JA Rosenberg… - Biochemistry, 2006 - ACS Publications
Prp19 is an essential splicing factor and a member of the U-box family of E3 ubiquitin
ligases. Prp19 forms a tetramer via a central coiled-coil domain. Here, we show the U-box …

[HTML][HTML] pSILAC mass spectrometry reveals ZFP91 as IMiD-dependent substrate of the CRL4CRBN ubiquitin ligase

J An, CM Ponthier, R Sack, J Seebacher… - Nature …, 2017 - nature.com
Thalidomide and its derivatives lenalidomide and pomalidomide (IMiDs) are effective
treatments of haematologic malignancies. It was shown that IMiDs impart gain-of-function …

[HTML][HTML] Plasticity of the Cullin-RING ligase repertoire shapes sensitivity to ligand-induced protein degradation

C Mayor-Ruiz, MG Jaeger, S Bauer, M Brand, C Sin… - Molecular cell, 2019 - cell.com
Inducing protein degradation via small molecules is a transformative therapeutic paradigm.
Although structural requirements of target degradation are emerging, mechanisms …

Recognition of substrate degrons by E3 ubiquitin ligases and modulation by small-molecule mimicry strategies

X Lucas, A Ciulli - Current opinion in structural biology, 2017 - Elsevier
Highlights•E3 ligases recruit substrates for proteasomal degradation by recognition of
degrons.•Crystal structures reveal the structural basis and mechanism of degron …

[HTML][HTML] SCFFbxo22-KDM4A targets methylated p53 for degradation and regulates senescence

Y Johmura, J Sun, K Kitagawa, K Nakanishi… - Nature …, 2016 - nature.com
Recent evidence has revealed that senescence induction requires fine-tuned activation of
p53, however, mechanisms underlying the regulation of p53 activity during senescence …

E3 ubiquitin ligase that recognizes sugar chains

Y Yoshida, T Chiba, F Tokunaga, H Kawasaki, K Iwai… - Nature, 2002 - nature.com
N-glycosylation of proteins in the endoplasmic reticulum (ER) has a central role in protein
quality control,,. Here we report that N-glycan serves as a signal for degradation by the Skp1 …

Targeting Cullin–RING E3 ubiquitin ligases for drug discovery: structure, assembly and small-molecule modulation

E Bulatov, A Ciulli - Biochemical Journal, 2015 - portlandpress.com
In the last decade, the ubiquitin–proteasome system has emerged as a valid target for the
development of novel therapeutics. E3 ubiquitin ligases are particularly attractive targets …